PF-4800567 - Casein Kinase 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEPF-4800567Cat. No.: HY-12470CAS No.: 1188296-52-7分式: CHClNO分量: 359.81作靶點(diǎn): Casein Kinase作通路: Cell Cycle/DNA Damage; Stem Cell/Wnt儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 75 mg/mL (208

2、.44 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 2.7792 mL 13.8962 mL 27.7924 mL5 mM 0.5558 mL 2.7792 mL 5.5585 mL10 mM 0.2779 mL 1.3896 mL 2.7792 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍福渲魄罢埾扰渲瞥吻宓膬湟?，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；

3、澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.95 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.95 mM); Clear solution3. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/

4、mL (6.95 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 PF-4800567種有效、選擇性的酪蛋激酶 1 (CK1) 抑制劑，IC50 值為 32 nM，對其選擇性是對 CK1 (IC50，711 nM) 的 20 倍。IC50 & Target CK1 CKI32 nM (IC50) 711 nM (IC50)體外研究 PF-4800567 is a potent and selective inhibitor of casein kinase 1

5、(CK1), with an IC50 of 32 nM, which isgreater than 20-fold selectivity over CK1 (IC50, 711 nM). PF-4800567 shows inhibitory activity against CK1and CK1 in whole cells, with IC50s of 2.65 and 20.38 M, respectively. PF-4800567 (0.01-10 M) blocksCK1-mediated PER3 nuclear localization mediated by CK1 an

6、d suppresses PER2 degradation at 1 M. Inaddition, PF-4800567 has little effect on the circadian clock at 32 nM 1.體內(nèi)研究 PF-4800567 (100 mg/kg, s.c.) is rapidly absorpted and distributed in plasma and brain of mice 1.PROTOCOLCell Assay 1 For drug treatment, 24 h after synchronization, individual dishes

7、 of cells under PMT recording are treatedwith CK1 inhibitors (PF-4800567 or PF-670462 at a range of doses) or DMSO (vehicle control). Thecompounds are left continuously with the samples thereafter, and the luminescence patterns are recorded forat least 6 days. Periods are analyzed by use of RAP soft

8、ware 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Walton KM, et al. Selective inhibition of casein kinase 1 epsilon minimally alters circadian clock period. J Pharmacol Exp Ther. 2009Aug;330(2):430-9.McePdfHeightCaution: Product has not been fully validated for medical applications.F